反应详情
EQUATION
反应方程式
REACTANTS
反应物
PRODUCTS
生成物
AUXILIARIES
试剂、催化剂与溶剂
CONDITIONS
反应条件
- 温度
- 150 °C
PROCEDURE
实验过程
A mixture of N-(5-bromo(1,3-thiazol-2-yl))(2-chlorophenyl)carboxamide (47, 62 mg, 0.2 mmol), (1-ethyl-3-(trifluoromethyl)-1H-pyrazol-5-yl)boronic acid (58) (62 mg, 0.3 mmol), [1,1′-bis(diphenylphosphino)ferrocene]palladium(II) chloride dichloromethane complex (1:1) (24 mg) and potassium phosphate (63 mg) in 2 ml DMA and 0.5 ml water was heated under Ar in microwave reactor at 150° C. for 30 min. The reaction mixture was worked up with EA/brine. Org. phase was concentrated and then subjected to prep HPLC purification to give 11.5 mg (2-chlorophenyl)-N-{5-[1-ethyl-3-(trifluoromethyl)pyrazol-5-yl](1,3-thiazol-2-yl)}carboxamide (59) as dark brown solid (yield: 14%; purity>90%). LC-MS: calcd. for C16H12ClF3N4OS: 401 (M+1).
WORKUP
后处理
- concentrationphase was concentrated
- customHPLC purification